Table 1.
Binding affinities to PKC δ and PKC βI for tigliane, ingenane, and bryostatin analogs and prodrugs
| PKC binding affinity, Ki | |
| 4 (parent) | 0.5 nM, 1.4 nM* |
| 6a | >2.5 µM† |
| 6b | >2.5 µM, >2.5 µM* |
| 6c | >2.5 µM† |
| 6d | >2.5 µM, >0.5 µM* |
| 6e | 380 nM† |
| 6f | >2.5 µM† |
| 9 (parent) | 1.1 nM, 0.85 nM* |
| 7 | >2.5 µM, >2.5 µM* |
| 1 (parent) | 1.1 nM, 2.2 nM* |
| 8a | >1 µM‡ |
| 8b | >5 µM‡ |
| 8c | 308 nM‡ |
| 8d | >5 µM‡ |
| 8e | >5 µM‡ |
Ki values are from a heterogeneous competitive binding assay against [3H]-phorbol dibutyrate.
Binding affinity to PKC δ and βI, respectively.
Binding affinity to PKC δ.
Binding affinity to PKC βI.